A single ascending-dose study of muscle regulator ace-031 in healthy volunteers
A single ascending-dose study of muscle regulator ace-031 in healthy volunteers
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DOI：
10.1002/mus.23539
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发表时间：
2013-03-01
期刊：
影响因子：
3.4
通讯作者：
Sherman, Matthew L.
中科院分区：
文献类型：
--
作者：
Attie, Kenneth M.;Borgstein, Niels G.;Sherman, Matthew L.
ACE-031是活化素受体IIB型（ActRIIB）的可溶性形式。ACE-031通过结合肌肉生长抑制素和其他肌肉质量的负调节剂来促进肌肉生长。方法本双盲、安慰剂对照研究在48名健康绝经后妇女中评价ACE-031的安全性、药代动力学和药效学，这些妇女随机接受1剂ACE-031（0.023 mg/kg SC）或安慰剂（3：1）。结果ACE-031的耐受性良好。不良事件包括注射部位红斑。平均ACE-031 AUC 0和Cmax随剂量线性增加;平均T1/2为1015天。第29天，在3 mg/kg组中观察到平均全身瘦体重（3.3%; P = 0.03，DXA）和大腿肌肉体积（5.1%; P = 0.03，MRI）统计学显著性增加。血清生物标志物的统计学显著变化表明ACE-031也改善了骨和脂肪代谢。结论：单剂量ACE-031治疗一般耐受性良好，并导致健康绝经后妇女肌肉质量增加。肌肉神经[B]47[/B]：416423，2013
Introduction ACE-031 is a soluble form of activin receptor type IIB (ActRIIB). ACE-031 promotes muscle growth by binding to myostatin and other negative regulators of muscle mass. Methods This double-blind, placebo-controlled study evaluated the safety, pharmacokinetics, and pharmacodynamics of ACE-031 in 48 healthy, postmenopausal women randomized to receive 1 dose of ACE-031 (0.023 mg/kg SC) or placebo (3:1). Results ACE-031 was generally well-tolerated. Adverse events included injection site erythema. Mean ACE-031 AUC0 and Cmax increased linearly with dose; mean T1/2 was 1015 days. Statistically significant increases in mean total body lean mass (3.3%; P = 0.03, by DXA) and thigh muscle volume (5.1%; P = 0.03, by MRI) were observed at day 29 in the 3 mg/kg group. Statistically significant changes in serum biomarkers suggest ACE-031 also improved bone and fat metabolism. Conclusions Single-dose ACE-031 treatment was generally well-tolerated and resulted in increases in muscle mass in healthy postmenopausal women. Muscle Nerve [B]47[/B]: 416423, 2013